US10130717B2ActiveUtilityA1

LHRH-platinum conjugates for treating reproductive cancers

Assignee: EASTERN KENTUCKY UNIVPriority: Dec 4, 2015Filed: Dec 2, 2016Granted: Nov 20, 2018
Est. expiryDec 4, 2035(~9.4 yrs left)· nominal 20-yr term from priority
C07F 15/0093A61K 47/48246A61K 33/24C07K 19/00A61K 47/64C07K 7/23A61K 33/243
77
PatentIndex Score
2
Cited by
49
References
16
Claims

Abstract

The conjugation of luteinizing hormone-releasing hormone (LHRH) with activated cisplatin using a malonate linker gives rise to a new Platinum-LHRH conjugate that effectively targets tumor cells that express the LHRH receptor. The Pt-LHRH conjugate may be used in a method for killing or inhibiting the growth of a tumor cell, especially in late state, highly invasive and aggressive stage IV tumors and in reoccurring tumors.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A compound having a structure: 
       
         
           
           
               
               
           
         
       
     
     
       2. A method for slowing the growth of cancer cells in a mammal; wherein the cancer cells express a receptor for luteinizing hormone-releasing hormone; the method comprising administering to the recipient an effective amount and an effective route of the compound of  claim 1 . 
     
     
       3. A method for lessening the incidents of metastasis of cancer cells in a mammal wherein the cancer cells express a receptor for luteinizing hormone-releasing hormone; the method comprising administering to the recipient an effective amount and an effective route of the compound of  claim 1 . 
     
     
       4. A compound comprising:
 a hormone domain comprising SEQ ID NO 1; 
 a platinum drug comprising activated cisplatin; 
 a linker comprising a malonate linker; 
 wherein SEQ ID NO 1 is conjugated to activated cisplatin utilizing the linker. 
 
     
     
       5. A compound comprising:
 a hormone domain comprising [D-Lys 6 ]-LHRH; 
 a platinum drug comprising activated cisplatin; 
 a linker comprising a malonate linker; 
 wherein [D-Lys 6 ]-LHRH is conjugated to activated cisplatin utilizing the linker. 
 
     
     
       6. A compound comprising:
 a hormone domain comprising [D-Trp 6 ]-LHRH; 
 a platinum drug comprising activated cisplatin; 
 a linker comprising a malonate linker; 
 wherein [D-Trp 6 ]-LHRH is conjugated to activated cisplatin utilizing the linker. 
 
     
     
       7. A compound comprising:
 a hormone domain comprising [D-Ala 6 ]-LHRH; 
 a platinum drug comprising activated cisplatin; 
 a linker comprising a malonate linker; 
 wherein [D-Ala 6 ]-LHRH is conjugated to activated cisplatin utilizing the linker. 
 
     
     
       8. A compound comprising:
 a hormone domain comprising buserelin; 
 a platinum drug comprising activated cisplatin; 
 a linker comprising a malonate linker; 
 wherein busrelin is conjugated to activated cisplatin utilizing the linker. 
 
     
     
       9. A compound comprising:
 a hormone domain comprising triptorelin; 
 a platinum drug comprising activated cisplatin; 
 a linker comprising a malonate linker; 
 wherein triptorelin is conjugated to activated cisplatin utilizing the linker. 
 
     
     
       10. A compound comprising:
 a hormone domain comprising gonadorelin; 
 a platinum drug comprising activated cisplatin; 
 a linker drug comprising a malonate linker; 
 wherein gonadorelin is conjugated to activated cisplatin utilizing the linker. 
 
     
     
       11. A compound comprising:
 a hormone domain comprising leuprorelin; 
 a platinum drug comprising activated cisplatin; 
 a linker comprising a malonate linker; 
 wherein leuprorelin is conjugated to activated cisplatin utilizing the linker. 
 
     
     
       12. A compound comprising:
 a hormone domain comprising [Gln 8 ]-LHRH; 
 a platinum drug comprising activated cisplatin; 
 a linker comprising a malonate linker; 
 wherein [Gln 8 ]-LHRH is conjugated to activated cisplatin utilizing the linker. 
 
     
     
       13. A method for slowing the growth of cancer cells in a mammal; wherein the cancer cells express a receptor for luteinizing hormone-releasing hormone; the method comprising administering to the recipient an effective amount and an effective route of the compound of  claim 4 . 
     
     
       14. A method for lessening the incidents of metastasis of cancer cells in a mammal wherein the cancer cells express a receptor for luteinizing hormone-releasing hormone; the method comprising administering to the recipient an effective amount and an effective route of the compound of  claim 4 . 
     
     
       15. A method for slowing the growth of cancer cells in a mammal; wherein the cancer cells express a receptor for luteinizing hormone-releasing hormone; the method comprising administering to the recipient an effective amount and an effective route of the compound of  claim 5 . 
     
     
       16. A method for lessening the incidents of metastasis of cancer cells in a mammal wherein the cancer cells express a receptor for luteinizing hormone-releasing hormone; the method comprising administering to the recipient an effective amount and an effective route of the compound of  claim 5 .

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